^
    3ms
    Focal adhesion kinase/Src family kinase axis-mediated tyrosine phosphorylation of metabolic enzymes facilitates tumor metastasis. (PubMed, Signal Transduct Target Ther)
    In the present study, we found that the tyrosine kinase complex-focal adhesion kinase (FAK)/Src family kinase (SFK) axis specifically contributes to metabolic reprogramming by inducing the phosphorylation of ATP-citrate synthase (ACLY) Tyr542, Tyr652, and fructose-bisphosphate aldolase A (ALDOA) Tyr174, Tyr302, or Tyr328 sites in both primary and metastatic ESCC cells...Moreover, it has been shown to have antitumor effects alone or in combination with FAK/SFK inhibitors both in vivo and in vitro. The inhibition of tyrosine kinase-regulated metabolic enzyme activities and related signaling networks may be a potential strategy for the treatment and diagnosis of metastatic ESCC.
    Journal
    |
    CDK7 (Cyclin Dependent Kinase 7) • ALDOA (Aldolase Fructose-Bisphosphate A)
    |
    TY-302
    4ms
    Study of TY-302 Capsules Combined With Abiraterone in Patients With Metastatic Castration-resistant Prostate Cancer（mCRPC） (clinicaltrials.gov)
    P1/2, N=48, Not yet recruiting, TYK Medicines, Inc
    New P1/2 trial
    |
    abiraterone acetate • TY-302
    over2years
    TY-2699a is a highly potent CDK7 inhibitor to abolish dysfunctional tumor cell cycle for clinical development (AACR 2023)
    Currently, trilaciclib, palbociclib, ribociclib, and abemaciclib that bear dual specificities against CDK4 and CDK6 have been approved for clinical usage, and more CDK4/6 targeted agents are actively under clinical evaluations, among which, TY-302, a novel CDK4/6 inhibitor being developed by TYK Medicines, is under Phase II trial (NCT04433494)...Several CDK7 targeted agents, such as SY-5609 and Samuraciclib (CT7001), are under development...# Shengli Dong and Apeng Liang contributed equally to this work. * Jun Li, Shengli Dong and Apeng Liang are the correspondent authors.
    Clinical • Tumor cell
    |
    CCND1 (Cyclin D1) • CCNE1 (Cyclin E1) • CCNA2 (Cyclin A2) • CDK2 (Cyclin-dependent kinase 2) • CDK7 (Cyclin Dependent Kinase 7) • CDK1 (Cyclin-dependent kinase 1)
    |
    CDK7 overexpression
    |
    Ibrance (palbociclib) • Verzenio (abemaciclib) • Kisqali (ribociclib) • Cosela (trilaciclib) • SY-5609 • samuraciclib (CT7001) • TY-2699a • TY-302
    almost3years
    A Study of TY-302 in Patients With Advanced Solid Tumors (clinicaltrials.gov)
    P1, N=60, Recruiting, TYK Medicines, Inc | Trial completion date: Dec 2022 --> Dec 2023 | Trial primary completion date: May 2022 --> May 2023
    Trial completion date • Trial primary completion date • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor)
    |
    HER-2 negative • PGR positive
    |
    tamoxifen • TY-302
    over3years
    A Study of TY-302 in Patients With Advanced Solid Tumors (clinicaltrials.gov)
    P1, N=60, Recruiting, TYK Medicines, Inc | Not yet recruiting --> Recruiting
    Enrollment open
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor)
    |
    HER-2 negative • PGR positive
    |
    tamoxifen • TY-302
    over5years
    A Study of TY-302 in Patients With Advanced Solid Tumors (clinicaltrials.gov)
    P1, N=60, Not yet recruiting, TYK Medicines, Inc
    Clinical • New P1 trial
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor)
    |
    HER-2 negative • PGR positive
    |
    tamoxifen • TY-302